SCH221510 [Ligand Id: 8868] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL513136
  • δ receptor/Delta opioid receptor in Human [ChEMBL: CHEMBL236] [GtoPdb: 317] [UniProtKB: P41143]
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  • κ receptor/Kappa opioid receptor in Human [ChEMBL: CHEMBL237] [GtoPdb: 318] [UniProtKB: P41145]
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  • μ receptor/Mu opioid receptor in Human [ChEMBL: CHEMBL233] [GtoPdb: 319] [UniProtKB: P35372]
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  • NOP receptor/Nociceptin receptor in Human [ChEMBL: CHEMBL2014] [GtoPdb: 320] [UniProtKB: P41146]
  • NOP receptor in Mouse [GtoPdb: 320] [UniProtKB: P35377]
  • NOP receptor in Rat [GtoPdb: 320] [UniProtKB: P35370]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
δ receptor/Delta opioid receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL236] [GtoPdb: 317] [UniProtKB: P41143]
GtoPdb Radioligand binding assay - 5.54 pKi 2854 nM Ki J Pharmacol Exp Ther (2008) 326: 672-82 [PMID:18492950]
ChEMBL Displacement of [3H]diprenorphine from human delta opioid receptor expressed in CHO cells B 5.54 pKi 2854 nM Ki Bioorg. Med. Chem. Lett. (2009) 19: 2519-2523 [PMID:19339177]
κ receptor/Kappa opioid receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL237] [GtoPdb: 318] [UniProtKB: P41145]
GtoPdb Radioligand binding assay - 6.88 pKi 131 nM Ki J Pharmacol Exp Ther (2008) 326: 672-82 [PMID:18492950]
ChEMBL Displacement of [3H]diprenorphine from human kappa opioid receptor expressed in CHO cells B 6.88 pKi 131 nM Ki Bioorg. Med. Chem. Lett. (2009) 19: 2519-2523 [PMID:19339177]
μ receptor/Mu opioid receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL233] [GtoPdb: 319] [UniProtKB: P35372]
ChEMBL Displacement of [3H]diprenorphine from human mu opioid receptor expressed in CHO cells B 7.19 pKi 65 nM Ki Bioorg. Med. Chem. Lett. (2009) 19: 2519-2523 [PMID:19339177]
GtoPdb Radioligand binding assay - 7.19 pKi 65 nM Ki J Pharmacol Exp Ther (2008) 326: 672-82 [PMID:18492950]
ChEMBL Agonist activity at human mu opioid assessed as stimulation of GDP-induced [35S]GTPgammaS binding F 6.16 pEC50 693 nM EC50 Bioorg. Med. Chem. Lett. (2009) 19: 2519-2523 [PMID:19339177]
NOP receptor/Nociceptin receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2014] [GtoPdb: 320] [UniProtKB: P41146]
GtoPdb Radioligand binding assay - 9.52 pKi 0.3 nM Ki J Pharmacol Exp Ther (2008) 326: 672-82 [PMID:18492950]
ChEMBL Displacement of [125I][Tyr14]nociceptin from human cloned NOP receptor expressed in CHO cells B 9.52 pKi 0.3 nM Ki Bioorg. Med. Chem. Lett. (2009) 19: 2519-2523 [PMID:19339177]
GtoPdb Stimulation of GTP-γ35S binding - 7.92 pEC50 12 nM EC50 J Pharmacol Exp Ther (2008) 326: 672-82 [PMID:18492950]
ChEMBL Agonist activity at human NOP assessed as stimulation of GDP-induced [35S]GTPgammaS binding F 7.92 pEC50 12 nM EC50 Bioorg. Med. Chem. Lett. (2009) 19: 2519-2523 [PMID:19339177]
NOP receptor in Mouse [GtoPdb: 320] [UniProtKB: P35377]
GtoPdb Radioligand binding assay - 8.94 pKi 1.15 nM Ki J Pharmacol Exp Ther (2008) 326: 672-82 [PMID:18492950]
NOP receptor in Rat [GtoPdb: 320] [UniProtKB: P35370]
GtoPdb Radioligand binding assay - 9.38 pKi 0.42 nM Ki J Pharmacol Exp Ther (2008) 326: 672-82 [PMID:18492950]

ChEMBL data shown on this page come from version 28:

Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, CibriƔn-Uhalte E, Davies M, Dedman N, Karlsson A, MagariƱos MP, Overington JP, Papadatos G, Smit I, Leach AR. (2017) 'The ChEMBL database in 2017.' Nucleic Acids Res., 45(D1). DOI: 10.1093/nar/gkw1074. [PMCID:5210557]